Quinazoline dione compounds and their uses

JP7858148B1Active Publication Date: 2026-05-13EDGEWISE THERAPEUTICS INC
View PDF 8 Cites 0 Cited by

Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Filing Date
2024-03-26
Publication Date
2026-05-13

AI Technical Summary

Benefits of technology

【0354】 また本明細書では、例えば、開示される化合物および追加の活性剤を、これらの治療剤の共同作用から有益な効果を提供することが意図された特定の処置レジメンの一部として併用投与する併用療法が企図される。組合せの有益な効果としては、それに限定されるものではないが、治療剤の組合せから生じる薬物動態または薬力学的共同作用が挙げられる。組合せにおけるこれらの治療剤の投与は、典型的に、規定された期間(通常、選択された組合せに応じて、数時間、数日、数週、数カ月または数年)にわたって行われる。併用療法は、逐次的方式での複数の治療剤の投与(すなわち、ここでは各治療剤が、異なる時点で投与される)、および実質的に同時方式でのこれらの治療剤または治療剤の少なくとも2つの投与を包含することを意図される。

✦ Generated by Eureka AI based on patent content.

Smart Images

  • Figure 0007858148000001
    Figure 0007858148000001
  • Figure 0007858148000002
    Figure 0007858148000002
  • Figure 0007858148000003
    Figure 0007858148000003
Patent Text Reader

Abstract

Quinazoline dione compounds are provided for treating cardiac indications such as hypertrophic cardiomyopathy and diastolic dysfunction. Diseases treated by the methods described herein include, but are not limited to, cardiomyopathy, hypertrophic cardiomyopathy (HCM), abnormal heart rhythms, aortic disease, Marfan syndrome, coronary artery disease, heart attack, heart failure, rheumatic heart disease, peripheral vascular disease, stroke, deep vein thrombosis, and pulmonary embolism.
Need to check novelty before this filing date? Find Prior Art

Claims

1. Equation (Ia): 【Chemistry 181】 A compound or salt thereof represented by formula (Ia): R ２ teeth: 【Chemistry 182】 Selected from; X １ is C(R １ａ ), N, and N ＋ (-O － ) are selected from; X ２ is selected from C(R １ｂ ), N, and N ＋ (-O － ); X ３ is C(R １ｃ ), N, and N ＋ (-O － ) are selected from; X ４ is C(R １ｄ ), N, and N ＋ (-O － ) are selected from; Here X １ , X ２ , X ３ , and X ４ Two or fewer of these are N or N ＋ (-O － ) and; Y １ N, and N ＋ (-O － ) are selected from; Y ２ is C(R ９ｂＢ ), N, and N ＋ (-O － ) are selected from; Y ３ is C(R ９ｂＣ ) are selected from; Y ４ is C(R ９ｂＤ ), N, and N ＋ (-O － ) are selected from; Y ５ is C(R ９ｂＥ ), N, and N ＋ (-O － ) are selected from; Here Y ２ , Y ４ , and Y ５ Two or fewer of these are N or N ＋ (-O － ) and; R １ａ , R １ｂ , and R1c are independent of each other: hydrogen; ハロゲン、-NO ２ 、-N ３ 、-CN、-OR １０ａ 、-SR １０ａ 、-N(R １０ａ ) ２ 、-C(O)R １０ａ 、-C(O)N(R １０ａ ) ２ 、-N(R １０ａ )C(O)R １０ａ 、-N(R １０ａ )C(O)N(R １０ａ ) ２ 、-OC(O)N(R １０ａ ) ２ 、-N(R １０ａ )C(O)OR １０ａ 、-C(O)OR １０ａ 、-OC(O)R １０ａ 、-S(O)R １０ａ 、および-S(O) ２ R １０ａ ; C １～６ alkyl, C ２～６ alkenyl, and C ２～６ alkynyl, each of which is halogen, -OR １０ａ , -SR １０ａ , -N(R １０ａ ), -C(O)R ２ , -C(O)N(R １０ａ ), -N(R １０ａ ), -N(R ２ ), -N(R １０ａ ), -C(O)R １０ａ , -C(O)OR １０ａ , -OC(O)R １０ａ , -N(R １０ａ ), -C(O)N(R １０ａ ), -OC(O)N(R ２ ), -N(R １０ａ ), -C(O)OR ２ , -N(R １０ａ ), -S(O)R １０ａ , -S(O)<( ２ R<( ２ R １０ａ , -NO ２ , =O, =S, =N(R １０ａ ), -N<( ３ , -CN, C ３～１０ carbocyclic ring and one or more substituents independently selected from 3- to 10-membered heterocyclic rings are optionally substituted, where each C ３～１０ carbocyclic ring and 3- to 10-membered heterocyclic ring are optionally substituted with one or more substituents independently selected from R ９ａ ; and C ３～１０ Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR １０ａ , -SR １０ａ , -N(R １０ａ ) ２ , -C(O)R １０ａ , -C(O)N(R １０ａ ) ２ , -N(R １０ａ ) C(O)R １０ａ , -N(R １０ａ ) C(O)N(R １０ａ ) ２ , -OC(O)N(R １０ａ ) ２ , -N(R １０ａ ) C(O)OR １０ａ , -C(O)OR １０ａ , -OC(O)R １０ａ , -S(O)R １０ａ , -S(O) ２ R １０ａ , -NO ２ , =O, =S, =N(R １０ａ ), -N ３ ,-CN,C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ It is optionally substituted with one or more substituents independently selected from the alkynyl, where each C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ Alkinyl is R ９ａ Substituted as needed with one or more substituents independently selected from Selected from; R 1d is: hydrogen; -NO 2 , -N 3 , -CN, -OR 10a , -SR 10a , -N(R 10a ) 2 , -C(O)R 10a , -C(O)N(R 10a ) 2 , -N(R 10a )C(O)R 10a , -N(R 10a )C(O)N(R 10a ) 2 , -OC(O)N(R 10a ) 2 , -N(R 10a )C(O)OR 10a , -C(O)OR 10a , -OC(O)R 10a , -S(O)R 10a , and -S(O) 2 R 10a ; C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl, each of which is a halogen, -OR 10a, -SR 10a, -N(R 10a)2, -C(O)R 10a, -C(O)N(R 10a)2, -N(R 10a)C(O)R 10a, -C(O)OR 10a, -OC(O)R 10a, -N(R 10a)C(O)N(R 10a)2, -OC(O)N(R 10a)2, -N(R 10a)C(O)OR 10a, -S(O)R 10a, -S(O)2R 10a, -NO2 ,=O,=S,=N(R 10a),-N3,-CN, optionally substituted with one or more substituents independently selected from C3-10 carbon rings and 3- to 10-membered heterocycles, where each C3-10 carbon ring and 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from R 9a; and C3-10 carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 10a, -SR 10a, -N(R 10a)2, -C(O)R 10a, -C(O)N(R 10a)2, -N(R 10a)C(O)R 10a, -N(R 10a)C(O)N(R 10a)2, -OC(O)N(R 10a)2, -N(R 10a)C(O)OR 10a, -C(O)OR 10a, -OC(O)R 10a, -S(O)R 10a, -S(O)2R 10a, -NO2 ,=O,=S,=N(R 10a),-N 3,-CN, optionally substituted with one or more substituents independently selected from C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl, where each C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl is optionally substituted with one or more substituents independently selected from R 9a. Selected from; R Ｚ teeth: -CN, -C(O)R １０ｚ , -C(O)N(R １０ｚ ) ２ , and -C(O)OR １０ｚ ; C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ Alkynnyl, each of which is a halogen, -OR １０ｚ , -SR １０ｚ , -N(R １０ｚ ) ２ , -C(O)R １０ｚ , -C(O)N(R １０ｚ ) ２ , -N(R １０ｚ ) C(O)R １０ｚ , -C(O)OR １０ｚ , -OC(O)R １０ｚ , -N(R １０ｚ ) C(O)N(R １０ｚ ) ２ , -OC(O)N(R １０ｚ ) ２ , -N(R １０ｚ ) C(O)OR １０ｚ , -S(O)R １０ｚ , -S(O) ２ R １０ｚ , -NO ２ , =O, =S, =N(R １０ｚ ), -N ３ ,-CN,C ３～１０ It is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles, where each C ３～１０ Carbon rings and 3- to 10-membered heterocycles are R ９ｚ Substituted as necessary with one or more substituents independently selected from; and C ３～１０ Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR １０ｚ , -SR １０ｚ , -N(R １０ｚ ) ２ , -C(O)R １０ｚ , -C(O)N(R １０ｚ ) ２ , -N(R １０ｚ ) C(O)R １０ｚ , -N(R １０ｚ ) C(O)N(R １０ｚ ) ２ , -OC(O)N(R １０ｚ ) ２ , -N(R １０ｚ ) C(O)OR １０ｚ , -C(O)OR １０ｚ , -OC(O)R １０ｚ , -S(O)R １０ｚ , -S(O) ２ R １０ｚ , -NO ２ , =O, =S, =N(R １０ｚ ), -N ３ ,-CN,C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ It is optionally substituted with one or more substituents independently selected from the alkynyl, where each C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ Alkinyl is R ９ｚ Substituted as needed with one or more substituents independently selected from Selected from; or R C, together with R Z, forms a 3- to 10-membered heterocycle or a C3- to 10-carbon ring, where the 3- to 10-membered heterocycle or C3- to 10-carbon ring is optionally substituted with one or more substituents independently selected from R 9c; R Ｃ teeth: hydrogen; -CN, -C(O)R １０ｃ , -C(O)N(R １０ｃ ) ２ , and -C(O)OR １０ｃ ; C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ Alkynnyl, each of which is a halogen, -OR １０ｃ , -SR １０ｃ , -N(R １０ｃ ) ２ , -C(O)R １０ｃ , -C(O)N(R １０ｃ ) ２ , -N(R １０ｃ ) C(O)R １０ｃ , -C(O)OR １０ｃ , -OC(O)R １０ｃ , -N(R １０ｃ ) C(O)N(R １０ｃ ) ２ , -OC(O)N(R １０ｃ ) ２ , -N(R １０ｃ ) C(O)OR １０ｃ , -S(O)R １０ｃ , -S(O) ２ R １０ｃ , -NO ２ , =O, =S, =N(R １０ｃ ), -N ３ ,-CN,C ３～１０ It is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles, where each C ３～１０ Carbon rings and 3- to 10-membered heterocycles are R ９ｃ Substituted as necessary with one or more substituents independently selected from; and C ３～１０ Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR １０ｃ , -SR １０ｃ , -N(R １０ｃ ) ２ , -C(O)R １０ｃ , -C(O)N(R １０ｃ ) ２ , -N(R １０ｃ ) C(O)R １０ｃ , -N(R １０ｃ ) C(O)N(R １０ｃ ) ２ , -OC(O)N(R １０ｃ ) ２ , -N(R １０ｃ ) C(O)OR １０ｃ , -C(O)OR １０ｃ , -OC(O)R １０ｃ , -S(O)R １０ｃ , -S(O) ２ R １０ｃ , -NO ２ , =O, =S, =N(R １０ｃ ), -N ３ ,-CN,C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ It is optionally substituted with one or more substituents independently selected from the alkynyl, where each C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ Alkinyl is R ９ｃ Substituted as needed with one or more substituents independently selected from Selected from; or R Ｚ is R Ｃ Together with it, a 3-membered to 10-membered hetero ring or C ３～１０ A carbon ring is formed, where the 3-membered to 10-membered heterocycle or C ３～１０ The carbon ring is R ９ｃ It is optionally substituted with one or more substituents selected independently of it; R ５ teeth: hydrogen; ハロゲン、-OR １０ｄ 、-SR １０ｄ 、-N(R １０ｄ ) ２ 、-C(O)R １０ｄ 、-C(O)N(R １０ｄ ) ２ 、-N(R １０ｄ )C(O)R １０ｄ 、-C(O)OR １０ｄ 、-OC(O)R １０ｄ 、-N(R １０ｄ )C(O)N(R １０ｄ ) ２ 、-OC(O)N(R １０ｄ ) ２ 、-N(R １０ｄ )C(O)OR １０ｄ 、-S(O)R １０ｄ 、-S(O) ２ R １０ｄ 、-NO ２ 、-N ３ 、および-CN; C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ Alkynnyl, each of which is a halogen, -OR １０ｄ , -SR １０ｄ , -N(R １０ｄ ) ２ , -C(O)R １０ｄ , -C(O)N(R １０ｄ ) ２ , -N(R １０ｄ ) C(O)R １０ｄ , -C(O)OR １０ｄ , -OC(O)R １０ｄ , -N(R １０ｄ ) C(O)N(R １０ｄ ) ２ , -OC(O)N(R １０ｄ ) ２ , -N(R １０ｄ ) C(O)OR １０ｄ , -S(O)R １０ｄ , -S(O) ２ R １０ｄ , -NO ２ , =O, =S, =N(R １０ｄ ), -N ３ ,-CN,C ３～１０ It is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles, where each C ３～１０ Carbon rings and 3- to 10-membered heterocycles are R ９ｄ Substituted as necessary with one or more substituents independently selected from; and C ３～１０ Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR １０ｄ , -SR １０ｄ , -N(R １０ｄ ) ２ , -C(O)R １０ｄ , -C(O)N(R １０ｄ ) ２ , -N(R １０ｄ ) C(O)R １０ｄ , -N(R １０ｄ ) C(O)N(R １０ｄ ) ２ , -OC(O)N(R １０ｄ ) ２ , -N(R １０ｄ ) C(O)OR １０ｄ , -C(O)OR １０ｄ , -OC(O)R １０ｄ , -S(O)R １０ｄ , -S(O) ２ R １０ｄ , -NO ２ , =O, =S, =N(R １０ｄ ), -N ３ ,-CN,C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ It is optionally substituted with one or more substituents independently selected from the alkynyl, where each C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ Alkinyl is R ９ｄ Substituted as needed with one or more substituents independently selected from Selected from; or R ５ is R ６ Together with it, a 3-membered to 10-membered hetero ring or C ３～１０ A carbon ring is formed, where the 3-membered to 10-membered heterocycle or C ３～１０ The carbon ring is R ９ｄ It is optionally substituted with one or more substituents selected independently of it; R ６ teeth: hydrogen; ハロゲン、-OR １０ｅ 、-SR １０ｅ 、-N(R １０ｅ ) ２ 、-C(O)R １０ｅ 、-C(O)N(R １０ｅ ) ２ 、-N(R １０ｅ )C(O)R １０ｅ 、-C(O)OR １０ｅ 、-OC(O)R １０ｅ 、-N(R １０ｅ )C(O)N(R １０ｅ ) ２ 、-OC(O)N(R １０ｅ ) ２ 、-N(R １０ｅ )C(O)OR １０ｅ 、-S(O)R １０ｅ 、-S(O) ２ R １０ｅ 、-NO ２ 、-N ３ 、および-CN; C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ Alkynnyl, each of which is a halogen, -OR １０ｅ , -SR １０ｅ , -N(R １０ｅ ) ２ , -C(O)R １０ｅ , -C(O)N(R １０ｅ ) ２ , -N(R １０ｅ ) C(O)R １０ｅ , -C(O)OR １０ｅ , -OC(O)R １０ｅ , -N(R １０ｅ ) C(O)N(R １０ｅ ) ２ , -OC(O)N(R １０ｅ ) ２ , -N(R １０ｅ ) C(O)OR １０ｅ , -S(O)R １０ｅ , -S(O) ２ R １０ｅ , -NO ２ , =O, =S, =N(R １０ｅ ), -N ３ ,-CN,C ３～１０ It is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles, where each C ３～１０ Carbon rings and 3- to 10-membered heterocycles are R ９ｅ Substituted as necessary with one or more substituents independently selected from; and C ３～１０ Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR １０ｅ , -SR １０ｅ , -N(R １０ｅ ) ２ , -C(O)R １０ｅ , -C(O)N(R １０ｅ ) ２ , -N(R １０ｅ ) C(O)R １０ｅ , -N(R １０ｅ ) C(O)N(R １０ｅ ) ２ , -OC(O)N(R １０ｅ ) ２ , -N(R １０ｅ ) C(O)OR １０ｅ , -C(O)OR １０ｅ , -OC(O)R １０ｅ , -S(O)R １０ｅ , -S(O) ２ R １０ｅ , -NO ２ , =O, =S, =N(R １０ｅ ), -N ３ ,-CN,C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ It is optionally substituted with one or more substituents independently selected from the alkynyl, where each C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ Alkinyl is R ９ｅ Substituted as needed with one or more substituents independently selected from Selected from; or R ６ is R ５ Together with it, a 3-membered to 10-membered hetero ring or C ３～１０ A carbon ring is formed, where the 3-membered to 10-membered heterocycle or C ３～１０ The carbon ring is R ９ｅ It is optionally substituted with one or more substituents selected independently of it; R ７ teeth: hydrogen; -C(O)R １０ｆ , -C(O)N(R １０ｆ ) ２ , -C(O)OR １０ｆ , -S(O)R １０ｆ , and -S(O) ２ R １０ｆ ; Halogen, -OR １０ｆ , -SR １０ｆ , -N(R １０ｆ ) ２ , -C(O)R １０ｆ , -C(O)N(R １０ｆ ) ２ , -N(R １０ｆ ) C(O)R １０ｆ , -C(O)OR １０ｆ , -OC(O)R １０ｆ , -N(R １０ｆ ) C(O)N(R １０ｆ ) ２ , -OC(O)N(R １０ｆ ) ２ , -N(R １０ｆ ) C(O)OR １０ｆ , -S(O)R １０ｆ , -S(O) ２ R １０ｆ , -NO ２ , =O, =S, =N(R １０ｆ ), -N ３ ,-CN,C ３～１０ C is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles. １～６ Alkyl, where each C ３～１０ Carbon rings and 3- to 10-membered heterocycles are R ９ｆ Substituted as necessary with one or more substituents independently selected from; and C ３～１０ Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR １０ｆ , -SR １０ｆ , -N(R １０ｆ ) ２ , -C(O)R １０ｆ , -C(O)N(R １０ｆ ) ２ , -N(R １０ｆ ) C(O)R １０ｆ , -N(R １０ｆ ) C(O)N(R １０ｆ ) ２ , -OC(O)N(R １０ｆ ) ２ , -N(R １０ｆ ) C(O)OR １０ｆ , -C(O)OR １０ｆ , -OC(O)R １０ｆ , -S(O)R １０ｆ , -S(O) ２ R １０ｆ , -NO ２ , =O, =S, =N(R １０ｆ ), -N ３ ,-CN,C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ It is optionally substituted with one or more substituents independently selected from the alkynyl, where each C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ Alkinyl is R ９ｆ Substituted as needed with one or more substituents independently selected from Selected from; R ８ teeth: hydrogen; -C(O)R １０ｇ , -C(O)N(R １０ｇ ) ２ , -C(O)OR １０ｇ , -S(O)R １０ｇ , and -S(O) ２ R １０ｇ ; Halogen, -OR １０ｇ , -SR １０ｇ , -N(R １０ｇ ) ２ , -C(O)R １０ｇ , -C(O)N(R １０ｇ ) ２ , -N(R １０ｇ ) C(O)R １０ｇ , -C(O)OR １０ｇ , -OC(O)R １０ｇ , -N(R １０ｇ ) C(O)N(R １０ｇ ) ２ , -OC(O)N(R １０ｇ ) ２ , -N(R １０ｇ ) C(O)OR １０ｇ , -S(O)R １０ｇ , -S(O) ２ R １０ｇ , -NO ２ , =O, =S, =N(R １０ｇ ), -N ３ ,-CN,C ３～１０ C is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles. １～６ Alkyl, where each C ３～１０ Carbon rings and 3- to 10-membered heterocycles are R ９ｇ Substituted as necessary with one or more substituents independently selected from; and C ３～１０ Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR １０ｇ , -SR １０ｇ , -N(R １０ｇ ) ２ , -C(O)R １０ｇ , -C(O)N(R １０ｇ ) ２ , -N(R １０ｇ ) C(O)R １０ｇ , -N(R １０ｇ ) C(O)N(R １０ｇ ) ２ , -OC(O)N(R １０ｇ ) ２ , -N(R １０ｇ ) C(O)OR １０ｇ , -C(O)OR １０ｇ , -OC(O)R １０ｇ , -S(O)R １０ｇ , -S(O) ２ R １０ｇ , -NO ２ , =O, =S, =N(R １０ｇ ), -N ３ ,-CN,C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ It is optionally substituted with one or more substituents independently selected from the alkynyl, where each C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ Alkinyl is R ９ｇ Substituted as needed with one or more substituents independently selected from Selected from; Each R ９ａ Independently: Halogen, -OR １０ａ , -SR １０ａ , -N(R １０ａ ) ２ , -C(O)R １０ａ , -C(O)N(R １０ａ ) ２ , -N(R １０ａ ) C(O)R １０ａ , -N(R １０ａ ) C(O)N(R １０ａ ) ２ , -OC(O)N(R １０ａ ) ２ , -N(R １０ａ ) C(O)OR １０ａ , -C(O)OR １０ａ , -OC(O)R １０ａ , -S(O)R １０ａ , -S(O) ２ R １０ａ , -NO ２ , =O, =S, =N(R １０ａ ), -N ３ , and -CN; and C １～３ Alkyl, C ２～３ Alkenyl and C ２～３ Alkynnyl, each of which is a halogen, -OR １０ａ , -SR １０ａ , -N(R １０ａ ) ２ , -C(O)R １０ａ , -C(O)N(R １０ａ ) ２ , -N(R １０ａ ) C(O)R １０ａ , -N(R １０ａ ) C(O)N(R １０ａ ) ２ , -OC(O)N(R １０ａ ) ２ , -N(R １０ａ ) C(O)OR １０ａ , -C(O)OR １０ａ , -OC(O)R １０ａ , -S(O)R １０ａ , -S(O) ２ R １０ａ , -NO ２ , =O, =S, =N(R １０ａ ), -N ３ , and which are optionally substituted with one or more substituents independently selected from -CN. Selected from; R ９ｂＢ , R ９ｂＤ , and R ９ｂＥ Each is independent of the others: hydrogen; ハロゲン、-NO ２ 、-N ３ 、-CN、-OR １０ｂ 、-SR １０ｂ 、-N(R １０ｂ ) ２ 、-C(O)R １０ｂ 、-C(O)N(R １０ｂ ) ２ 、-N(R １０ｂ )C(O)R １０ｂ 、-N(R １０ｂ )C(O)N(R １０ｂ ) ２ 、-OC(O)N(R １０ｂ ) ２ 、-N(R １０ｂ )C(O)OR １０ｂ 、-C(O)OR １０ｂ 、-OC(O)R １０ｂ 、-S(O)R １０ｂ 、および-S(O) ２ R １０ｂ ; C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ Alkynnyl, each of which is a halogen, -OR １０ｂ , -SR １０ｂ , -N(R １０ｂ ) ２ , -C(O)R １０ｂ , -C(O)N(R １０ｂ ) ２ , -N(R １０ｂ ) C(O)R １０ｂ , -C(O)OR １０ｂ , -OC(O)R １０ｂ , -N(R １０ｂ ) C(O)N(R １０ｂ ) ２ , -OC(O)N(R １０ｂ ) ２ , -N(R １０ｂ ) C(O)OR １０ｂ , -S(O)R １０ｂ , -S(O) ２ R １０ｂ , -NO ２ , =O, =S, =N(R １０ｂ ), -N ３ ,-CN,C ３～１０ Carbocyclic rings, and those optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles; and C ３～１０ Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR １０ｂ , -SR １０ｂ , -N(R １０ｂ ) ２ , -C(O)R １０ｂ , -C(O)N(R １０ｂ ) ２ , -N(R １０ｂ ) C(O)R １０ｂ , -N(R １０ｂ ) C(O)N(R １０ｂ ) ２ , -OC(O)N(R １０ｂ ) ２ , -N(R １０ｂ ) C(O)OR １０ｂ , -C(O)OR １０ｂ , -OC(O)R １０ｂ , -S(O)R １０ｂ , -S(O) ２ R １０ｂ , -NO ２ , =O, =S, =N(R １０ｂ ), -N ３ ,-CN,C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ Substituted as needed with one or more substituents independently selected from the alkynyl group. Selected from; R 9bC is: Halogen, -NO 2 , -N 3 , -CN, -OR 10b , -SR 10b , -N(R 10b ) 2 , -C(O)R 10b , -C(O)N(R 10b ) 2 , -N(R 10b )C(O)R 10b , -N(R 10b )C(O)N(R 10b ) 2 , -OC(O)N(R 10b ) 2 , -N(R 10b )C(O)OR 10b , -C(O)OR 10b , -OC(O)R 10b , -S(O)R 10b , and -S(O) 2 R 10b ; C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl, each of which is a halogen, -OR 10b, -SR 10b, -N(R 10b)2, -C(O)R 10b, -C(O)N(R 10b)2, -N(R 10b)C(O)R 10b, -C(O)OR 10b, -OC(O)R 10b, -N(R 10b)C(O)N(R 10b)2, -OC(O)N(R 10b)2, -N(R 10b)C(O)OR 10b, -S(O)R 10b, -S(O)2R 10b, -NO2 ,=O,=S,=N(R 10b),-N3,-CN,C3-10 carbon rings, and 3-membered-to-10-membered heterocycles, which are optionally substituted with one or more substituents independently selected from these; and C3-10 carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 10b, -SR 10b, -N(R 10b)2, -C(O)R 10b, -C(O)N(R 10b)2, -N(R 10b)C(O)R 10b, -N(R 10b)C(O)N(R 10b)2, -OC(O)N(R 10b)2, -N(R 10b)C(O)OR 10b, -C(O)OR 10b, -OC(O)R 10b, -S(O)R 10b, -S(O)2R 10b, -NO2 Substituted as necessary with one or more substituents independently selected from ,=O,=S,=N(R 10b),-N3,-CN, C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl Selected from; Each R ９ｚ Independently: Halogen, -OR １０ｚ , -SR １０ｚ , -N(R １０ｚ ) ２ , -C(O)R １０ｚ , -C(O)N(R １０ｚ ) ２ , -N(R １０ｚ ) C(O)R １０ｚ , -N(R １０ｚ ) C(O)N(R １０ｚ ) ２ , -OC(O)N(R １０ｚ ) ２ , -N(R １０ｚ ) C(O)OR １０ｚ , -C(O)OR １０ｚ , -OC(O)R １０ｚ , -S(O)R １０ｚ , -S(O) ２ R １０ｚ , -NO ２ , =O, =S, =N(R １０ｚ ), -N ３ , and -CN; and C １～３ Alkyl, C ２～３ Alkenyl and C ２～３ Alkynnyl, each of which is a halogen, -OR １０ｚ , -SR １０ｚ , -N(R １０ｚ ) ２ , -C(O)R １０ｚ , -C(O)N(R １０ｚ ) ２ , -N(R １０ｚ ) C(O)R １０ｚ , -N(R １０ｚ ) C(O)N(R １０ｚ ) ２ , -OC(O)N(R １０ｚ ) ２ , -N(R １０ｚ ) C(O)OR １０ｚ , -C(O)OR １０ｚ , -OC(O)R １０ｚ , -S(O)R １０ｚ , -S(O) ２ R １０ｚ , -NO ２ , =O, =S, =N(R １０ｚ ), -N ３ , and which are optionally substituted with one or more substituents independently selected from -CN. Selected from; Each R ９ｃ Independently: Halogen, -OR １０ｃ , -SR １０ｃ , -N(R １０ｃ ) ２ , -C(O)R １０ｃ , -C(O)N(R １０ｃ ) ２ , -N(R １０ｃ ) C(O)R １０ｃ , -N(R １０ｃ ) C(O)N(R １０ｃ ) ２ , -OC(O)N(R １０ｃ ) ２ , -N(R １０ｃ ) C(O)OR １０ｃ , -C(O)OR １０ｃ , -OC(O)R １０ｃ , -S(O)R １０ｃ , -S(O) ２ R １０ｃ , -NO ２ , =O, =S, =N(R １０ｃ ), -N ３ , and -CN; and C １～３ Alkyl, C ２～３ Alkenyl and C ２～３ Alkynnyl, each of which is a halogen, -OR １０ｃ , -SR １０ｃ , -N(R １０ｃ ) ２ , -C(O)R １０ｃ , -C(O)N(R １０ｃ ) ２ , -N(R １０ｃ ) C(O)R １０ｃ , -N(R １０ｃ ) C(O)N(R １０ｃ ) ２ , -OC(O)N(R １０ｃ ) ２ , -N(R １０ｃ ) C(O)OR １０ｃ , -C(O)OR １０ｃ , -OC(O)R １０ｃ , -S(O)R １０ｃ , -S(O) ２ R １０ｃ , -NO ２ , =O, =S, =N(R １０ｃ ), -N ３ , and which are optionally substituted with one or more substituents independently selected from -CN. Selected from; Each R ９ｄ Independently: Halogen, -OR １０ｄ , -SR １０ｄ , -N(R １０ｄ ) ２ , -C(O)R １０ｄ , -C(O)N(R １０ｄ ) ２ , -N(R １０ｄ ) C(O)R １０ｄ , -N(R １０ｄ ) C(O)N(R １０ｄ ) ２ , -OC(O)N(R １０ｄ ) ２ , -N(R １０ｄ ) C(O)OR １０ｄ , -C(O)OR １０ｄ , -OC(O)R １０ｄ , -S(O)R １０ｄ , -S(O) ２ R １０ｄ , -NO ２ , =O, =S, =N(R １０ｄ ), -N ３ , and -CN; and C １～３ Alkyl, C ２～３ Alkenyl and C ２～３ Alkynnyl, each of which is a halogen, -OR １０ｄ , -SR １０ｄ , -N(R １０ｄ ) ２ , -C(O)R １０ｄ , -C(O)N(R １０ｄ ) ２ , -N(R １０ｄ ) C(O)R １０ｄ , -N(R １０ｄ ) C(O)N(R １０ｄ ) ２ , -OC(O)N(R １０ｄ ) ２ , -N(R １０ｄ ) C(O)OR １０ｄ , -C(O)OR １０ｄ , -OC(O)R １０ｄ , -S(O)R １０ｄ , -S(O) ２ R １０ｄ , -NO ２ , =O, =S, =N(R １０ｄ ), -N ３ , and which are optionally substituted with one or more substituents independently selected from -CN. Selected from; Each R ９ｅ Independently: halogen, -OR １０ｅ , -SR １０ｅ , -N(R １０ｅ ), ２ , -C(O)R １０ｅ , -C(O)N(R １０ｅ ), ２ , -N(R １０ｅ ),C(O)R １０ｅ , -N(R １０ｅ ),C(O)N(R １０ｅ ), ２ , -OC(O)N(R １０ｅ ), ２ , -N(R １０ｅ ),C(O)OR １０ｅ , -C(O)OR １０ｅ , -OC(O)R １０ｅ , -S(O)R １０ｅ , -S(O) ２ R １０ｅ , -NO ２ , =O, =S, =N(R １０ｅ ), -N ３ , and -CN; and C １～３ alkyl, C ２～３ alkenyl, and C ２～３ alkynyl, each of which is halogen, -OR １０ｅ , -SR １０ｅ , -N(R １０ｅ ), -C(O)R ２ , -C(O)N(R １０ｅ ), -N(R １０ｅ ), -N(R ２ ), -N(R １０ｅ ), -N(R １０ｅ ), -N(R １０ｅ ), -N(R １０ｅ ), -OC(O)N(R ２ ), -N(R １０ｅ ), -N(R ２ ), -N(R １０ｅ ), -C(O)OR １０ｅ , -C(O)OR １０ｅ , -OC(O)R １０ｅ , -S(O)R １０ｅ , -S(O) ２ R １０ｅ , -NO ２ , =O, =S, =N(R １０ｅ ), -N ３ , and -CN, and is optionally substituted with one or more substituents independently selected therefrom Selected from; Each R ９ｆ Independently: Halogen, -OR １０ｆ , -SR １０ｆ , -N(R １０ｆ ) ２ , -C(O)R １０ｆ , -C(O)N(R １０ｆ ) ２ , -N(R １０ｆ ) C(O)R １０ｆ , -N(R １０ｆ ) C(O)N(R １０ｆ ) ２ , -OC(O)N(R １０ｆ ) ２ , -N(R １０ｆ ) C(O)OR １０ｆ , -C(O)OR １０ｆ , -OC(O)R １０ｆ , -S(O)R １０ｆ , -S(O) ２ R １０ｆ , -NO ２ , =O, =S, =N(R １０ｆ ), -N ３ , and -CN; and C １～３ alkyl, C ２～３ alkenyl, and C ２～３ alkynyl, each of which is halogen, -OR １０ｆ , -SR １０ｆ , -N(R １０ｆ ), -C(O)R ２ , -C(O)N(R １０ｆ ), -N(R １０ｆ ), -N(R ２ ), -N(R １０ｆ ), -N(R １０ｆ ), -N(R １０ｆ ), -N(R １０ｆ ), -OC(O)N(R ２ ), -N(R １０ｆ ), -N(R ２ ), -N(R １０ｆ ), -C(O)OR １０ｆ , -C(O)OR １０ｆ , -OC(O)R １０ｆ , -S(O)R １０ｆ , -S(O) ２ R １０ｆ , -NO ２ , =O, =S, =N(R １０ｆ ), -N ３ , and -CN, optionally substituted with one or more substituents independently selected from these Selected from; Each R ９ｇ Independently: Halogen, -OR １０ｇ , -SR １０ｇ , -N(R １０ｇ ) ２ , -C(O)R １０ｇ , -C(O)N(R １０ｇ ) ２ , -N(R １０ｇ ) C(O)R １０ｇ , -N(R １０ｇ ) C(O)N(R １０ｇ ) ２ , -OC(O)N(R １０ｇ ) ２ , -N(R １０ｇ ) C(O)OR １０ｇ , -C(O)OR １０ｇ , -OC(O)R １０ｇ , -S(O)R １０ｇ , -S(O) ２ R １０ｇ , -NO ２ , =O, =S, =N(R １０ｇ ), -N ３ , and -CN; and C １～３ Alkyl, C ２～３ Alkenyl and C ２～３ Alkynnyl, each of which is a halogen, -OR １０ｇ , -SR １０ｇ , -N(R １０ｇ ) ２ , -C(O)R １０ｇ , -C(O)N(R １０ｇ ) ２ , -N(R １０ｇ ) C(O)R １０ｇ , -N(R １０ｇ ) C(O)N(R １０ｇ ) ２ , -OC(O)N(R １０ｇ ) ２ , -N(R １０ｇ ) C(O)OR １０ｇ , -C(O)OR １０ｇ , -OC(O)R １０ｇ , -S(O)R １０ｇ , -S(O) ２ R １０ｇ , -NO ２ , =O, =S, =N(R １０ｇ ), -N ３ , and which are optionally substituted with one or more substituents independently selected from -CN. Selected from; and Each R １０ａ , R １０ｂ , R １０ｚ , R １０ｃ , R １０ｄ , R １０ｅ , R １０ｆ , and R １０ｇ Independently: hydrogen; C １～６ Alkyl, C ２～６ Alkenyl and C ２～６ Alkynnyl, each of which is a halogen, -CN, -OH, -SH, -NO ２ , -NH ２ , =O, =S, -OC １～６ Alkyl, -S-C １～６ Alkyl, -N(C) １～６ Alkyl) ２ ,-NH(C １～６ Alkyl), C ３～１０ Carbocyclic rings, and those optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles; and C ３～１０ Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, or -NO. ２ , -NH ２ , =O, =S, -OC １～６ Alkyl, -S-C １～６ Alkyl, -N(C) １～６ Alkyl) ２ ,-NH(C １～６ Alkyl), C １～６ Alkyl, C ２～６ Alkenil, C ２～６ Alkinyl, C ３～１０ Carbon rings, 3-membered to 10-membered heterocycles, and C １～６ Substituted as needed with one or more substituents independently selected from the haloalkyl group. A compound or a salt thereof, selected from the following.

2. X １ However, C(R １ａ ) will be selected from; X2 is selected from C(R1b); X 3 is selected from C (R 1c); The compound or salt according to claim 1, wherein X4 is selected from C(R1d).

3. The compound or salt according to Claim 1, wherein three or fewer of X1, X2, X3, and X4 are C(H).

4. X １ However, C(H), C(F), and C(CN), and C(CH) ３ ) will be selected from; X2 is selected from N, C(H), C(F), C(CH3), and C(CN); X 3 is C(H); and A compound or salt according to any one of claims 1 to 3, wherein X4 is C(H).

5. The compound or salt according to any one of claims 1 to 3, wherein one or less of Y2, Y4, and Y5 is N or N+ (-O-).

6. R １ａ , R １ｂ , and R1c each independently: hydrogen; Halogen, -NO ２ -CN, -OR １０ａ , -SR １０ａ , and -N(R １０ａ ) ２ ; and Halogen, -OR １０ａ , -SR １０ａ , -N(R １０ａ ) ２ , -NO ２ C as needed, substituted with one or more substituents independently selected from ,=O and -CN １～６ Alkyl A compound or salt according to any one of claims 1 to 3, selected from the above.

7. R １ａ , R １ｂ , and R1c are independently: hydrogen, halogen, -CN, and C １～６ A compound or salt according to any one of claims 1 to 3, selected from alkyl groups.

8. R 1d is: hydrogen; -NO 2, -CN, -OR 10a, -SR 10a, and -N(R 10a) 2; and C1-6 alkyl groups optionally substituted with one or more substituents independently selected from halogens, -OR 10a, -SR 10a, -N(R 10a)2, -NO2, =O, and -CN. A compound or salt according to any one of claims 1 to 3, selected from the above.

9. The compound or salt according to any one of claims 1 to 3, wherein R1d is selected from hydrogen, -CN, and C1-6 alkyl.

10. The compound or salt according to any one of claims 1 to 3, wherein R 1d is selected from hydrogen.

11. The compound or salt according to any one of claims 1 to 3, wherein Y1 is N.

12. R Ｚ ga: halogen, -OR １０ｚ , and C as needed, substituted with one or more substituents independently selected from -OH. １～６ A compound or salt according to any one of claims 1 to 3, selected from alkyl groups.

13. R Ｚ The compound or salt according to any one of claims 1 to 3, wherein the compound is selected from -CH3 and the R C is selected from hydrogen.

14. R Ｃ A compound or salt according to any one of claims 1 to 3, selected from hydrogen.

15. R ５ R ６ The compound or salt according to any one of claims 1 to 3, which together with the other to form a cyclopropyl group.

16. R ５ is hydrogen, and R ６ A compound or salt according to any one of claims 1 to 3, wherein the compound is hydrogen.

17. R ７ A compound or salt according to any one of claims 1 to 3, wherein hydrogen is selected.

18. The compound or salt according to any one of claims 1 to 3, wherein R7 is hydrogen and R8 is hydrogen.

19. Y2 is C(R 9bB), Y4 is C(R 9bD), and Y5 is C(R 9bE); or Y2 is C(R 9bB), Y4 is C(R 9bD), and Y5 is N; or A compound or salt according to any one of claims 1 to 3, wherein Y2 is N, Y4 is C(R9bD), and Y5 is C(R9bE).

20. Y ２ However, C(H), C(F), C(CH) ３ ), and selected from N; R 9bC is selected from -CN, -F, -Cl, and -OH; Y4 is selected from C(H), C(F), C(CH3), and N; and The compound or salt according to any one of claims 1 to 3, wherein Y5 is selected from N, C(H), C(F), and C(CH3).

21. The compound or salt according to any one of claims 1 to 3, wherein R 9bC is selected from -CN.

22. The compound or salt according to any one of claims 1 to 3, wherein Y2 is selected from C(H).

23. Y ３ The compound or salt according to any one of claims 1 to 3, wherein the compound is selected from N, C(H), C(CN), C(F), C(Cl), and C(OH).

24. Y ３ The compound or salt according to claim 23, selected from C(CN).

25. Y ４ However, C(H), C(F), C(CH) ３ A compound or salt according to any one of claims 1 to 3, selected from ), and N.

26. Y ５ However, N, C(H), C(F), and C(CH) ３ A compound or salt according to any one of claims 1 to 3, selected from ).

27. R ２ but, 【Chemistry 183】 A compound or salt according to any one of claims 1 to 3, selected from the above.

28. R2 is: 【Chemical 301】 A compound or salt according to any one of claims 1 to 3, selected from the above.

29. R2 is: 【Chemical 302】 A compound or salt according to any one of claims 1 to 3, selected from the above.

30. R ８ A compound or salt according to any one of claims 1 to 3, selected from hydrogen.

31. R ９ｂＢ , R ９ｂＤ , and R ９ｂＥ Each independently: hydrogen; halogen, -CN, -OR １０ｂ , -SR １０ｂ , and -N(R １０ｂ ) ２ ; and halogen, -OR １０ｂ , -SR １０ｂ , -N(R １０ｂ ) ２ C as needed, substituted with one or more substituents independently selected from ,=O and -CN １～６ A compound or salt according to any one of claims 1 to 3, selected from alkyl groups.

32. R ９ｂＢ , R ９ｂＤ , and R ９ｂＥ Each of these is independently: hydrogen, fluoro, -CN, -OH, and C １ A compound or salt according to any one of claims 1 to 3, selected from alkyl groups.

33. The compound or salt according to any one of claims 1 to 3, wherein R9bC is selected from fluoro, -CN, -OH, and C1 alkyl.

34. The compound or salt according to any one of claims 1 to 3, wherein R 9bC is -CN.

35. Each R ９ｚ , R ９ｃ , R 9d, R ９ｅ , R ９ｆ , and R ９ｇ The compound or salt according to any one of claims 1 to 3, wherein R10a, R10b, R10z, R10c, R10d, R10e, R10f, and R10g are independently selected from hydrogen and C1-6 alkyl.

36. Each R １０ａ , R １０ｂ , R １０ｚ , R １０ｃ , R １０ｄ , R １０ｅ , R １０ｆ , and R １０ｇ A compound or salt according to any one of claims 1 to 3, wherein the compound is independently selected from hydrogen.

37. Compound 【Chemical 303】 【Chemical 304】 【Chemical 305】 【Chemical 306】 【Chemical 307】 Or a compound or salt according to any one of claims 1 to 3, selected from any one of these salts.

38. The compound is 【Chemical 308】 The compound or salt thereof according to claim 1.

39. The compound is 【Chemical 309】 The compound or salt thereof according to claim 1.

40. The compound is 【Chemical 310】 The compound or salt thereof according to claim 1.

41. The compound is 【Chemical 311】 The compound or salt thereof according to claim 1.

42. The compound is 【Chemical 312】 The compound or salt thereof according to claim 1.

43. The compound is 【Chemistry 313】 The compound or salt thereof according to claim 1.

44. The compound is 【Chemical 314】 The compound or salt thereof according to claim 1.

45. The compound is 【Chemical Industry 315】 The compound or salt thereof according to claim 1.

46. The compound is 【Chemical 316】 The compound or salt thereof according to claim 1.

47. The compound is 【Chemical 317】 The compound or salt thereof according to claim 1.

48. A pharmaceutical composition comprising a compound or salt according to any one of claims 1 to 3 or any one of claims 38 to 47 and a pharmaceutically acceptable additive.